Assay Detail
Binding
CHEMBL748540
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Tested for inhibitory concentration against [3H]U-69593 binding at sites of kappa-opioid receptor in guinea pig brain membrane
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Cavia porcellus |
| Tissue | Brain |
| Subcellular | Membrane |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
Isothiocyanate-substituted kappa-selective opioid receptor ligands derived from N-methyl-N-[(1S)-1-phenyl-2-(1-pyrrolidinyl)ethyl] phenylacetamide.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 8 | 8.26 | 8.85 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL94734 | — | — | 1 | 8.85 |
| CHEMBL38576 | ICI-199,441 | — | 1 | 8.82 |
| CHEMBL95654 | — | — | 1 | 8.74 |
| CHEMBL440765 | U-69593 | — | 1 | 8.68 |
| CHEMBL97246 | — | — | 1 | 8.48 |
| CHEMBL95001 | — | — | 1 | 8.02 |
| CHEMBL124283 | — | — | 1 | 6.22 |
| CHEMBL31421 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL94734 | — | IC50 | = | 1.4 | nM | 8.85 |
| CHEMBL38576 | ICI-199,441 | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL95654 | — | IC50 | = | 1.8 | nM | 8.74 |
| CHEMBL440765 | U-69593 | IC50 | = | 2.1 | nM | 8.68 |
| CHEMBL97246 | — | IC50 | = | 3.3 | nM | 8.48 |
| CHEMBL95001 | — | IC50 | = | 9.5 | nM | 8.02 |
| CHEMBL124283 | — | IC50 | = | 600.0 | nM | 6.22 |
| CHEMBL31421 | — | IC50 | > | 1000.0 | nM | - |